| Autor: |
Spletstoser, J. T., Flaherty, P. T., Himes, R. H., Georg, G. I. |
| Zdroj: |
Journal of Medicinal Chemistry; December 2004, Vol. 47 Issue: 26 p6459-6465, 7p |
| Abstrakt: |
The synthesis and biological evaluation of a novel paclitaxel photoaffinity probe is described. The synthesis involved the preparation of an azide-containing C13 side chain through a Staudinger cycloaddition followed by a lipase-mediated kinetic resolution to obtain the azetidinone in 99% ee. Coupling of the enantiopure side chain precursor to 7-TES-baccatin III and subsequent silyl ether deprotection afforded 3-(4-azidophenyl)-3-dephenylpaclitaxel, which was shown to be as active as paclitaxel in tubulin assembly and cytotoxicity assays. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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